Synthesis and antifungal activity of camphoric acid-based acylhydrazone compounds
Synthesis and antifungal activity of camphoric acid-based acylhydrazone compounds
复制标题
樟脑酸基酰腙类化合物的合成及其抗真菌活性
DOI：
10.1515/hf-2014-0002
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发表时间：
2014-12-01
期刊：
影响因子：
2.4
通讯作者：
Lei, Fu-Hou
中科院分区：
文献类型：
--
作者：
Ma, Xian-Li;Li, Fang-Yao;Lei, Fu-Hou
为了寻找新的有效的生物活性化合物，以n -氨基樟脑酰亚胺(3)与以樟脑酸为原料的取代苯甲醛缩合反应为原料，设计并合成了18个新的基于樟脑酸的酰基腙化合物4a-4r。通过傅里叶变换红外（FTIR）、H-1核磁共振（NMR）、C-13核磁共振（NMR）、电喷雾电离质谱（ESI-MS）和元素分析对目标化合物进行了表征。初步生物实验表明，在50 μ g ml（-1）的浓度下，以樟脑酸为基础的化合物对梨状Physalospora piricola的抑制率为95%，分别为邻溴苯酰腙（4f）、对溴苯酰腙（4g）、对甲氧基苯酰腙（4m）和对羟基苯基酰腙（4p）。
In the search of novel potent bioactive compounds, 18 novel camphoric acid-based acylhydrazone compounds 4a-4r were designed and synthesized by the condensation reaction of N-amino camphorimide (3) with substituted benzaldehyde based on camphoric acid as the starting material. The target compounds were characterized by means of Fourier transform infrared (FTIR), H-1 nuclear magnetic resonance (NMR), C-13 NMR, electrospray ionization-mass spectrometry (ESI-MS), and elemental analysis. The preliminary bioassay showed that the following camphoric acid-based compounds exhibited excellent antifungal activity with an inhibition ratio of 95% against Physalospora piricola at the concentration of 50 mu g ml(-1): o-bromophenyl acylhydrazone (4f), p-bromophenyl acylhydrazone (4g), p-methoxyphenyl acylhydrazone (4m), and p-hydroxyphenyl acylhydrazone (4p).